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Catalog No.
Product Name
Application
Product Information
Citations
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CDK2 Inhibitor
CDK2-IN-55 is a selective CDK2 inhibitor with an IC50 value of 4.7 nM, also exhibiting significant inhibitory action on CDK1 (IC50 = 26.3 nM), alongside moderate inhibition of Aurora A (IC50 = 92.0 nM) and CDK9 (IC50 = 288 nM). Its weak inhibitory profile on CDK4, CDK6, DYRK1A, and GSK3β (IC50 > 1000 nM) highlights its specificity. CDK2-IN-55 demonstrates potent anti-proliferative effects against various cancer cell lines, effectively inducing cell cycle arrest and apoptosis, making it a valuable tool for research related to colorectal, lung, and cervical cancers. -
Cdk1 Inhibitor
BMI-1026 is a potent cyclin-dependent kinase 1 (Cdk1) inhibitor with an IC50 of 2.3 nM. This compound effectively induces apoptosis by interfering with cell cycle progression, specifically by causing a G2-M phase arrest. Its ability to modulate Cdk1 activity makes BMI-1026 valuable for research applications focused on cell division, cancer biology, and therapeutic strategies targeting cell cycle dysregulation. -
CDK1 Inhibitor
CDK1-IN-8 is a potent inhibitor of Cyclin-dependent kinase 1 (CDK1), primarily targeting the regulation of cell cycle progression. This compound effectively inhibits cell migration, induces apoptosis, and causes cell cycle arrest at the G2/M phase. Notably, CDK1-IN-8 leads to significant downregulation of CDK1 protein levels in HepG2 cells, making it a valuable tool for investigating mechanisms in hepatocellular carcinoma research. -
PKMYT1 Inhibitor
PD-166285 is a potent inhibitor of PKMYT1, exhibiting an IC50 value of 17 nM. This compound demonstrates significant antiproliferative activity against CCNE1-amplified cancer cell lines, including OVCAR3 (IC50 = 0.14 μM) and HCC1569 (IC50 = 0.21 μM). In addition to its antiproliferative effects, PD-166285 induces apoptosis and effectively arrests CCNE1-amplified HCC1569 cells in the G1/S phase of the cell cycle. This reagent serves as a valuable tool for exploring PKMYT1-targeted therapies in the context of CCNE1-amplified malignancies. -
CDK7 Inhibitor
SY-5102 is a potent and selective inhibitor of cyclin-dependent kinase 7 (CDK7) with a Kd of 0.03 nM. This compound exhibits significant anti-proliferative activity in HCC70 cells, with an EC50 of 9 nM, and effectively modulates CDK7-mediated functions, including downregulation of CDK2 Thr160 and RNA polymerase II Ser5 phosphorylation. SY-5102 induces G2/M cell cycle arrest and decreases c-Myc oncogene expression, leading to enhanced apoptosis in cancer cells. It is particularly relevant for research focused on triple-negative breast cancer (TNBC). -
CDKs Inhibitor
ZLWT-37 is a potent, orally active inhibitor of cyclin-dependent kinases (CDKs), specifically exhibiting IC50 values of 0.002 μM against CDK9 and 0.054 μM against CDK2. This compound effectively induces apoptosis and arrests the cell cycle at the G2/M phase in HCT116 cells. ZLWT-37 is valuable for researching CDK-related pathways and investigating therapeutic strategies in cancer treatment. -
CDK4 Inhibitor
ZDLD13 is a selective inhibitor of Cyclin-Dependent Kinase 4 (CDK4) with an IC50 of 0.38 μM. This β-carboline compound demonstrates potent anti-cancer activity against HCT116 cells, effectively inhibiting colony formation, invasion, and migration, while also inducing apoptosis and G1 phase cell cycle arrest. Additionally, ZDLD13 significantly inhibits tumor growth in HCT116 tumor xenograft models, making it a valuable tool for cancer research. -
CDK1 Inhibitor
CGP-74514 hydrochloride is a highly selective inhibitor of cyclin-dependent kinase 1 (CDK1) with an IC50 of 25 nM. By inhibiting the CDK1/cyclin B complex, it effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in tumor cells. This compound shows potential for use in research related to bladder cancer and other malignancies driven by CDK1 deregulation. -
KRASG12C Inhibitor
KRASG12C IN-19 is a selective inhibitor that targets the KRASG12C mutation. It demonstrates potent antiproliferative effects against KRASG12C-mutant non-small cell lung cancer (NSCLC) cell line H358, with an IC50 of 7.6 nM, and effectively inhibits downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN-19 shows minimal inhibitory activity against KRASG12V and KRASG12D mutants, with IC50 values exceeding 10,000 nM. This reagent forms a covalent bond with KRASG12V-GDP and provides a robust tool for research on KRASG12C-driven malignancies, including NSCLC, pancreatic cancer, and colorectal cancer. -
c-Myc Inhibitor
KSI-3716 is a potent c-Myc inhibitor that disrupts the binding of c-Myc to MAX, preventing the transcription of target genes. This compound serves as an effective agent in intravesical chemotherapy for bladder cancer, demonstrating significant antitumor activity. Its ability to modulate c-Myc signaling makes it a valuable tool for research into cancer biology and potential therapeutic interventions. -
Chk1 Inhibitor
Graviquinone is a selective Chk1 inhibitor that demonstrates potent cytotoxic effects across multiple cancer cell lines. This compound is particularly notable for its ability to circumvent ABCB1-mediated multidrug resistance while selectively inducing DNA damage in cancer cells. Additionally, Graviquinone enhances its cytotoxic potential by elevating reactive oxygen species (ROS) levels, making it a valuable tool for studying mechanisms of cancer treatment and DNA damage response. Its unique properties position Graviquinone as an effective reagent for cancer research applications. -
PDE2/CDK2 Inhibitor
Aristolochic acid D is a selective inhibitor of PDE2 with an IC50 of 4.673 μM and CDK2 with an IC50 of 25 μM, derived from Aristolochia indica L. This compound demonstrates significant anti-inflammatory properties while exhibiting a non-carcinogenic and non-nephrotoxic profile. Aristolochic acid D is valuable for research applications focused on inflammation and tumor-related diseases, offering insights into therapeutic strategies. -
SHP2/CDK4 Inhibitor
SHP2/CDK4-IN-1 is a potent dual inhibitor of SHP2 and CDK4, exhibiting IC50 values of 4.3 nM and 18.2 nM, respectively. This compound effectively induces G0/G1 phase cell cycle arrest, thereby inhibiting the proliferation of triple-negative breast cancer (TNBC) cell lines. In preclinical studies, SHP2/CDK4-IN-1 demonstrated significant antitumor efficacy in the EMT6 syngeneic mouse model, making it a valuable tool for research on TNBC. -
CDK1/CDK2 Inhibitor
K00546 is a highly selective inhibitor of cyclin-dependent kinases CDK1 and CDK2, exhibiting IC50 values of 0.6 nM and 0.5 nM, respectively, for CDK1/cyclin B and CDK2/cyclin A complexes. In addition, K00546 effectively inhibits CDC2-like kinases CLK1 and CLK3, with IC50 values of 8.9 nM and 29.2 nM, respectively. This compound is valuable for research focused on cell cycle regulation and the mechanistic study of kinase activity in cancer biology. -
Aurora/VEGF/PDGF Inhibitor
Ilorasertib hydrochloride is a potent, orally active inhibitor targeting Aurora kinases, with IC50 values of 116 nM, 5 nM, and 1 nM for Aurora A, B, and C, respectively. Additionally, it exhibits significant inhibition of VEGF and PDGF pathways. This compound is valuable for research related to acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS), facilitating studies into the mechanisms of these hematologic malignancies. -
CDK Inhibitor
GW297361 is an oxindole compound identified as a cyclin-dependent kinase (CDK) inhibitor with a selective action on Pho85 in cellular systems. It demonstrates significant inhibitory effects on yeast Cdk1 and Pho85, exhibiting IC50 values of 20 nM and 400 nM, respectively. This compound is valuable for research applications focused on cell cycle regulation and the study of kinase signaling pathways. -
DYRK1A Inhibitor
GNF2133 is a potent and selective inhibitor of DYRK1A, exhibiting an IC50 of 0.0062 µM for DYRK1A, with minimal activity against GSK3β (>50 µM). This compound has demonstrated significant proliferation potency and efficacy in both rat and human primary β-cells. GNF2133 notably enhances glucose disposal capacity and stimulates insulin secretion, making it a valuable reagent for research into type 1 diabetes. -
DYRK1A Inhibitor
AO-365/43472821 is a selective inhibitor of Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), with an IC50 of 0.29 μM, and demonstrates potent inhibition of CLK1 (IC50 = 0.08 μM). This compound has been shown to protect the human neuroblastoma cell line SH-SY5Y from Okadaic acid-induced cytotoxicity. Furthermore, AO-365/43472821 effectively reduces the expression levels of phosphorylated tau (pSer396) and Aβ1-42 proteins, making it a valuable reagent for research related to Alzheimer’s disease. -
DYRK1A Inhibitor
Atalaphyllidine is a selective inhibitor of DYRK1A kinase, demonstrating an IC50 of 2.2 μM. This natural product, derived from the stem bark of Glycosmis chlorosperma, plays a significant role in regulating protein phosphorylation, making it valuable in studies related to neurodegenerative diseases. Its specific mechanism of action positions Atalaphyllidine as a useful tool in understanding the pharmacological modulation of DYRK1A and its implications in various cellular processes. -
DYRK1A/GSK3β Inhibitor
GNF4877 is a potent dual inhibitor of DYRK1A and GSK3β, demonstrating IC50 values of 6 nM and 16 nM, respectively. This inhibition results in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and promotes β-cell proliferation, with an EC50 of 0.66 μM in mouse β (R7T1) cells. GNF4877 serves as a valuable tool in research related to diabetes and T-cell signaling pathways. -
Dyrk1A And Dyrk1B Inhibitor
INDY is a potent Dyrk1A and Dyrk1B inhibitor, acting as an ATP-competitive antagonist with IC50 values of 0.24 μM and 0.23 μM, respectively. By binding to the ATP pocket of these kinases, INDY exhibits a Ki of 0.18 μM for Dyrk1A. This compound significantly diminishes the self-renewal capacity of both normal and tumorigenic cells, making it a valuable tool for research in glioblastoma and neural progenitor cell studies. -
DYRK1A Inhibitor
DYRK1-IN-1 is a selective inhibitor of the DYRK1A kinase, exhibiting an IC50 value of 220 nM for its phosphorylation activity. It serves as a valuable chemical probe for investigating DYRK1A's role in the central nervous system. This compound is suitable for research applications focused on neurological disorders and the modulation of kinase-mediated signaling pathways. -
DYRK Inhibitor
Protein Kinase Inhibitor 1 Hydrochloride is a selective inhibitor targeting dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). It demonstrates potent inhibition with IC50 values of 136 nM for HIPK1 and 74 nM for HIPK2, alongside a Kd of 9.5 nM for HIPK2. This compound is suitable for studies exploring the role of HIPK family kinases in various signaling pathways and disease models, particularly in cancer research and cellular response to stress. -
Dyrk1B Kinase Inhibitor
AZ-Dyrk1B-33 is a potent and selective DYRK1B kinase inhibitor, exhibiting an IC50 of 7 nM. This compound effectively modulates DYRK1B activity, making it a valuable tool for investigating its role in cellular processes. AZ-Dyrk1B-33 is applicable in studies related to neurodegenerative diseases and cancer research, where DYRK1B activity is implicated. -
DYRK1A/DYRK2 Inhibitor
Dyrk1A-IN-4 is a selective DYRK1A and DYRK2 inhibitor, known for its potent activity with IC50 values of 2 nM and 6 nM, respectively. This compound effectively inhibits DYRK1A autophosphorylation at pSer520 in U2OS cells, displaying an IC50 of 28 nM. Dyrk1A-IN-4 is useful for investigating the roles of DYRK1A in various cancer types, including ovarian adenocarcinoma, neuroblastoma, and cervical squamous cell carcinoma. -
DYRK1A Inhibitor
Dyrk1A-IN-5 is a potent and selective inhibitor of DYRK1A, exhibiting an IC50 of 6 nM. It demonstrates notable selectivity for DYRK1B and CLK1, with IC50 values of 600 nM and 500 nM, respectively, while showing minimal activity against DYRK2 (IC50 > 10 μM). This compound is particularly valuable for research related to Down syndrome, facilitating the exploration of DYRK1A's role in cellular mechanisms associated with this condition. -
DYRK2 Inhibitor
YK-2-69 is a potent and selective inhibitor of DYRK2, exhibiting an IC50 value of 9 nM. It specifically targets Lys-231 and Lys-234 within the DYRK2 protein, making it a valuable tool for investigating the role of DYRK2 in cellular processes. This compound is primarily utilized in research focused on prostate cancer, providing insights into tumor biology and potential therapeutic strategies. -
DYRK1A Inhibitor
Dyrk1A-IN-3 is a selective inhibitor of the dual-specificity tyrosine-regulated kinase 1A (DYRK1A), exhibiting a binding affinity with an IC50 of 76 nM. This compound is valuable for investigations into neurodegenerative disorders, including Alzheimer's Disease, Huntington's Disease, and Parkinson's Disease. Researchers can utilize Dyrk1A-IN-3 to explore the role of DYRK1A in neuronal signaling and disease pathology. -
Casein Kinase/DYRK/TNIK Inhibitor
ON 108600 is a potent inhibitor of casein kinase 2 (CK2), TYRK1 (DYRK), and TNIK, demonstrating IC50 values of 0.016 μM against DYRK1A, 0.007 μM against DYRK2, 0.05 μM against CK2α1, 0.005 μM against CK2α2, and 0.005 μM against TNIK. This compound exhibits promising antitumor activity, making it a valuable tool for research applications focused on cancer biology, signaling pathways, and kinase inhibition studies. Its specificity for these kinases positions ON 108600 as a critical reagent for investigating therapeutic strategies targeting kinase-related diseases. -
DYRK1A Inhibitor
7-Deazaguanine is a selective inhibitor of DYRK1A, a kinase implicated in various neurological disorders and cancer. This compound demonstrates good blood-brain barrier penetration, making it suitable for studies related to Down's syndrome and oncogenic processes. Its unique properties facilitate research into the therapeutic potential of targeting DYRK1A in these contexts. -
DYRK/CLK Inhibitor
Leucettinib-92 is a selective inhibitor of DYRK and CLK kinases, demonstrating IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, and 124 nM for DYRK1A, among others. This compound exhibits significant biological activity by modulating kinase signaling pathways, making it a valuable tool for research in oncology and neurodegenerative diseases. Its potency against key kinases provides potential insights into therapeutic targeting and intervention strategies in various cellular processes. -
DYRK1A/1B Inhibitor
EHT 5372 is a potent and selective inhibitor of the DYRK family of kinases, demonstrating IC50 values of 0.22 nM for DYRK1A and 0.28 nM for DYRK1B. It exhibits notable inhibition against other members of the DYRK family and related kinases, making it a valuable tool for investigating the role of DYRKs in cellular signaling pathways. EHT 5372 is primarily utilized in research applications focused on neurodegenerative diseases and cancer, facilitating studies on cell proliferation, differentiation, and apoptosis. -
DYRK1A Inhibitor
GNF2133 hydrochloride is a selective and orally active inhibitor of DYRK1A, exhibiting an IC50 of 0.0062 µM for DYRK1A while remaining inactive against GSK3β at concentrations exceeding 50 µM. This compound demonstrates significant efficacy in enhancing proliferation and functioning of both rat and human primary β-cells. Additionally, GNF2133 hydrochloride enhances glucose disposal and promotes insulin secretion, making it a valuable tool for research in type 1 diabetes. -
DYRKs Inhibitor
DYRKs-IN-1 hydrochloride is a selective inhibitor of Dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), showing IC50 values of 5 nM for DYRK1A and 8 nM for DYRK1B. This compound exhibits antitumor activity, making it a valuable tool for cancer research. Its ability to modulate kinase activity positions it as a significant reagent for studying the role of DYRKs in oncogenesis and therapeutic interventions. -
DYRK1A Inhibitor
RD0392 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) with an IC50 of 1.3 nM. It exhibits significant potential in the study of neurodegenerative diseases, particularly Alzheimer's disease, by modulating pathways involved in neuroprotection and neuronal function. This compound is a valuable tool for researchers exploring the therapeutic implications of DYRK1A inhibition in neurodegenerative conditions. -
CDK/DYRK Inhibitor
ML 315 hydrochloride is a selective dual inhibitor targeting cyclin-dependent kinases (CDKs) and dual-specificity tyrosine-regulated kinases (DYRKs), exhibiting IC50 values of 68 nM and 282 nM, respectively. This compound is utilized in research focused on cancer and neurological diseases, providing insights into cell cycle regulation and neurodegenerative pathways. ML 315's potent inhibitory action makes it a valuable tool for studying therapeutic strategies in these critical areas. -
DYRK Inhibitor
Protein Kinase Inhibitor 1 is a selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), demonstrating an IC50 of 74 nM and a Kd of 9.5 nM. This compound is instrumental in the investigation of DYRK1A's role in various cellular processes, including neurodevelopment and cancer progression. It serves as a valuable tool for research applications focused on kinase signaling pathways and their implications in disease states. -
CDK Inhibitor
(R)-(+)-O-Demethylbuchenavianine is a selective inhibitor of Cyclin-dependent kinases (CDKs), specifically targeting CDK1 and CDK5 with IC50 values of 1.1 and 0.95 μM, respectively. Additionally, it shows inhibitory activity against glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1), and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), though with IC50 values greater than 10 μM. This compound is important for research focused on cell cycle regulation, cancer therapeutics, and neurodegenerative diseases. -
CDK/DYRK Inhibitor
ML 315 is a selective dual inhibitor of cyclin-dependent kinases (CDK) and dual-specificity tyrosine phosphorylation-regulated kinase (DYRK), exhibiting IC50 values of 68 nM and 282 nM, respectively. It demonstrates significant biological activity in modulating cell cycle progression and neuronal signaling pathways. This compound has applications in cancer research and the study of neurological diseases, facilitating insights into therapeutic targets within these areas. -
DYRKs Inhibitor
DYRKs-IN-1 is a potent inhibitor of dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), effectively targeting DYRK1A and DYRK1B with IC50 values of 5 nM and 8 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and potential therapeutic applications. Its specificity and efficacy support further investigations into the role of DYRKs in cell signaling and tumor progression. -
DYRK1A/DYRK1B Inhibitor
Dyrk1A/B-IN-1 is a selective inhibitor targeting DYRK1A and DYRK1B, exhibiting Kis of 67.8 nM and 237.9 nM, and IC50s of 1.1 μM and 0.8 μM, respectively. This compound is cell-permeable and non-toxic to human cells, making it suitable for investigating the cellular functions of DYRK1A and DYRK1B. Dyrk1A/B-IN-1 is valuable for research applications focused on understanding the role of these kinases in various pathological conditions. -
DYRK Inhibitor
TSL2109 is a selective DYRK2 and CDK4/6 inhibitor, exhibiting an IC50 of 22 nM for DYRK2. This compound induces cell cycle arrest and apoptosis in vitro, effectively suppressing tumor growth in the context of Enzalutamide resistance. TSL2109 demonstrates a safety profile suitable for research applications in prostate and breast cancer studies, highlighting its potential as a therapeutic agent in oncology. -
DYRK2 Inhibitor
DYRK2-IN-2 is a selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2), exhibiting an IC50 of 40.3 nM. This compound demonstrates low inhibitory activity against other DYRK family members and CDC-like kinases, making it a specific tool for studying DYRK2. DYRK2-IN-2 effectively inhibits tau protein phosphorylation at Thr212 and exhibits moderate cytotoxicity in HT22 neuronal cells. This reagent is valuable for investigating the role of DYRK2 in cancer biology and neurodegenerative diseases. -
Dyrk1A/α-syn Inhibitor
Dyrk1A/α-synuclein-IN-1 is an inhibitor targeting both Dyrk1A and α-synuclein aggregation, demonstrating IC50 values of 177 nM and 10.5 µM, respectively. This dual-action compound is noted for its potential neuroprotective effects and favorable central nervous system penetration. It is applicable in research surrounding neurodegenerative diseases and the modulation of protein aggregation pathways. -
DYRK Inhibitor
Dyrk1A-IN-1 is a selective inhibitor of Dyrk1A kinase activity, demonstrating an IC50 of 119 nM. This compound effectively inhibits the aggregation of tau and α-synuclein oligomers, making it a valuable tool for investigating neurodegenerative diseases. Its capacity to modulate kinase activity and prevent protein aggregation highlights its potential in studying pathways associated with tauopathies and synucleinopathies. -
Dyrk1A/α-syn Inhibitor
Dyrk1A/α-synuclein-IN-2 is an effective inhibitor targeting both Dyrk1A and α-synuclein aggregation, with an IC50 value of 7.8 µM for α-synuclein. This compound demonstrates significant potential for central nervous system (CNS) penetration and exhibits neuroprotective properties. It is particularly useful in research focused on neurodegenerative diseases and understanding the molecular mechanisms underlying α-synuclein pathology. -
DYRK1A Inhibitor
Aristolactam A IIIa functions as a DYRK1A inhibitor and is derived from the alkaloid structure found in Glycosmis chlorosperma. This compound demonstrates significant inhibition of platelet aggregation induced by arachidonic acid, collagen, and platelet-activating factor. Additionally, Aristolactam A IIIa exhibits potent cytotoxic effects on HeLa cells, making it a valuable tool for research in cancer biology and cellular signaling pathways. -
DYRK1A/B Inhibitor
JH-XIV-68-3 is a selective inhibitor of DYRK1A and DYRK1B, targeting these kinases to modulate downstream signaling pathways. This compound exhibits significant antitumor activity in head and neck squamous cell carcinoma (HNSCC) cell lines, making it a valuable tool for cancer research. Its specificity for DYRK1A and DYRK1B is confirmed through biochemical and cellular assays, supporting its potential in therapeutic applications targeting these kinases. -
DYRK Inhibitor
DYRKs-IN-2 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) family members, exhibiting IC50 values of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its selective inhibition of DYRKs enables exploration of their roles in cellular signaling pathways and therapeutic potential in oncology. -
Dyrk1A Inhibitor
AnnH31 is a selective inhibitor of Dyrk1A with an IC50 value of 81 nM. In addition, AnnH31 inhibits monoamine oxidase A (MAO-A) at an IC50 of 3.2 μM. This compound has been shown to reduce cell viability in HeLa, PC12, and SH-SY5Y cell lines, making it a valuable tool for research focused on neurodegeneration and cancer biology.
